Supersaturation technologies

Overview

Laboratoria Smeets has hotmelt technology at low temperatures that can improve water solubility of API’s and hence enhance bioavailability.

Supersaturation is particularly useful applications where blended powders are to be administered via sachets dissolved in tap water or added to drinking water dosage systems in veterinary applications.

Supersaturated powders and solutions

A supersaturated solution contains more absorbable material than could be dissolved under normal circumstances.

Previously, the main problem in boosting saturation has been that where free drug concentrations rise above equilibrium solubility, this leads to drug precipitation or crystallization.

Recently, it has been established that certain polymers can maintain drug supersaturation after dispersion or digestion of the vehicle, leading to improvements in bioavailability and variability in exposure.

LabSmeets can improve the stability of supersaturated solutions using three principal mechanisms:

• increasing temperature to create more thermic movement
• using polymeric precipitation inhibitors (PPIs) and excipients, such as PEG 400, Tween or HPMC

Supersaturation mechanisms

LaboSmeets incorporation of crystallization inhibitors in blended powders and sachet-delivered drugs can work via four main mechanisms.

In the first place, the inhibitors reduce the crystallization rate of drugs, increasing stability.

Second, the inhibitors provide a steric barrier to drug molecules and inhibit crystallization through specific intermolecular interactions on growing crystal surfaces.

Third, they encourage adsorption onto faces of host crystals, reducing the crystal growth rate of the host and producing smaller crystal creases.

Finally, under very high supersaturated states, nucleation can be accelerated, leading to smaller crystals better able to stay in suspension. Polymeric stabilizers increase the nucleation rate by lowering the interfacial tension and encouraging adsorption to particle surfaces to inhibit growth through condensation and coagulation, again enhancing stability.

Packaging and blending advantages

Laboratoria Smeets can apply supersaturation technologies to a wide range of blended powders, liquids and semi-solids, along with tablets, capsules and sachet-delivered products.

Supersaturation technologies can deliver products that have greater bioavailability, enhanced stability and a more balanced response to variability in exposure.

Quality

Laboratoria Smeets NV is certificated for cGMP production and licensed for psychotropic and narcotic drugs. Quality management systems are based on EU GMP legislation and guidelines, backed up by regular internal and external inspection and audits.

Resources

Click on Supersaturation technologies for other information.
Click on LabSmeets to contact the company directly.

Sources

WARREN, D.B et al. (2010) Using polymeric precipitation inhibitors to improve the absorption of poorly water-soluble drugs: A mechanistic basis for utility. Journal of Drug Targeting. 18 (10).p.704–731.

3 MATTEUCCI, M.A. (2007) Highly Supersaturated Aqueous Solutions by Design of Amorphous Pharmaceutical Nanoparticles. University of Texas, Ph.D Dissertation

Supplier Information
Supplier: Laboratoria Smeets S.A
Address: Fotografielaan 42, 3040 Wilrijk, Belgium
Tel: +32 3828 2937
Fax: +32 3830 2136
Website: www.labosmeets.com